专利号:US-5623068-A 优先权日:1994-03-07 标 题:Synthesis of DNA using substituted phenylacetyl-protected nucleotides 发明人:REDDY M PARAMESWARA; FAROOQUI FIRDOUS; HANNA NAEEM B 权利人:BECKMAN INSTRUMENTS INC 摘要:Deoxyribonucleotide and ribonucleotide derivatives of the general formula I I wherein R1 represents -CR'R''-Ar, in which Ar is substituted aryl (as hereinafter defined) and R' and R'' are independently selected from the group consisting of hydrogen and lower alkyl; one of -R2 and R3 is a hydroxyl-protecting group and the other is a group suitable for synthesis of polynucleotides or for attachment of the nucleotide to a solid support; R4 is selected from the group consisting of hydrogen, -OH and protected hydroxyl; and B represents a divalent radical corresponding to a purine or pyrimidine base. When synthesis is carried out using these derivatives, the deprotection procedure is reduced to an essentially instantaneous process. The derivatives have acceptable shelf life and are very stable to conventional DNA synthesis conditions. Particularly preferred are those compounds wherein Ar is mono- and dihalo-substituted phenyl.
专利号:US-7098354-B2 优先权日:2002-10-25 标 题:Racemoselective synthesis of rac-diorganosilylbis(2-methylbenzo[e]indeyl)zirconium compounds 发明人:DAMRAU HANS-ROBERT; MUELLER PATRIK; GARCIA VALERIE; SIDOT CHRISTIAN; TELLIER CHRISTIAN; LELONG JEAN-FRANCOIS 权利人:BASELL POLYOLEFINE GMBH 摘要:The present invention relates to a specific process for the diastereoselective synthesis of rac-diorganosilylbis(2-methylbenzo[e]indenyl)zirconium compounds of the formula I, n nby reacting the silyl-bridged bisindenyl ligand with a dihalozirconium bis(3,5-di-tert-butylphenoxide)-base adduct to form the diorganosilylbis(2-methylbenzo[e]indenyl)zirconium bis(3,5-di-tert-butylphenoxide) and subsequently replacing the phenoxide groups by X using suitable replacement reagents to give the compound of the formula I; where the substituents X can be identical or different and are each F, Cl, Br, I or linear, cyclic or branched C 1-10 -alkyl; and the substituents R can be identical or different and are each linear, cyclic or branched C 1-10 -alkyl or C 6-10 -aryl; and also to the use of these compounds as catalysts.
专利号:US-6413957-B1 优先权日:1998-04-21 标题:Methods of inhibiting cell proliferation using indeno [1,2-c]pyrazol-4-ones 发明人:NUGIEL DAVID A; CARINI DAVID J; DI MEO SUSAN V; YUE EDDY W 权利人:BRISTOL MYERS SUIBB PHARMA COM 摘要:The present invention relates to the synthesis of a new class of indeno[1,2-c]pyrazol-4-ones of formula (I): n that are potent inhibitors of the class of enzymes known as cyclin dependent kinases, which relate to the catalytic subunits cdk1-7 and their regulatory subunits know as cyclins A-G. This invention also provides a novel method of treating cancer or other proliferative diseases by administering a therapeutically effective amount of one of these compounds or a pharmaceutically acceptable salt form thereof. Alternatively, one can treat cancer or other proliferative diseases by administering a therapeutically effective combination of one of the compounds of the present invention and one or more other known anti-cancer or anti-proliferative agents.
专利号:US-8481501-B2 优先权日:2004-05-28 标 题 :Synthesis of metabolically stable analgesics, pain medications and other agents 发明人:CASHMAN JOHN R; MACDOUGALL JAMES M 权利人:CASHMAN JOHN R; MACDOUGALL JAMES M; HUMAN BIOMOLECULAR RES INST 摘要:Disclosed are analgesic-related compositions and methods of using the compositions for modulation of analgesic receptor activity. The compositions and methods are useful for reducing pain, as well as for therapeutic intervention of addictions or other diseases or disorders amenable to treatment or prophylaxis by modulation of analgesic receptor signaling.
专利号:US-7250435-B2 优先权日:1999-10-20 标 题:Acylsemicarbazides as cyclin dependent kinase inhibitors useful as anti-cancer and anti-proliferative agents 发明人:NUGIEL DAVID A; CARINI DAVID J; DI MEO SUSAN V; VIDWANS ANUP P; YUE EDDY 权利人:BRISTOL MYERS SQUIBB PHARMA CO 摘要:The present invention relates to the synthesis of a new class of indeno[1,2-c]pyrazol-4-ones of formula (I): n nthat are potent inhibitors of the class of enzymes known as cyclin dependent kinases, which relate to the catalytic subunits cdk1-7 and their regulatory subunits know as cyclins A-G.n n This invention also provides a novel method of treating cancer or other proliferative diseases by administering a therapeutically effective amount of one of these compounds or a pharmaceutically acceptable salt form thereof. Alternatively, one can treat cancer or other proliferative diseases by administering a therapeutically effective combination of one of the compounds of the present invention and one or more other known anti-cancer or anti-proliferative agents.
专利号:US-7193099-B2 优先权日:2002-10-25 标 题:Racemoselective preparation of isolable ansa-metallocene biphenoxide complexes 发明人:DAMRAU HANS-ROBERT-HELLMUTH; MUELLER PATRIK; GARCIA VALERIE; SIDOT CHRISTIAN; TELLIER CHRISTIAN; LELONG JEAN-FRANCOIS 权利人:BASELL POLYOLEFINE GMBH 摘要:The invention relates to a process for preparing racemic metallocene biphenoxide complexes by reacting bridged transition metal complexes with cyclopentadienyl derivatives of alkali metals or alkaline earth metals and heating the reaction mixture obtained in this way to a temperature in the range from −78 to 250° C., to the corresponding metallocene biphenoxide complexes and to their use as catalysts or as constituents of catalysts for the polymerization of olefinically unsaturated compounds or as reagents or catalysts in stereoselective synthesis.
参考文献:10.1007/bf00406242 摘要:Schneider MR, Schönenberger H, Michel RT, Fortmeyer HP. Synthesis and evaluation of catechol analogs of diethylstilbestrol on a hormone-dependent human mammary carcinoma implanted in nude mice. Journal of Cancer Research and Clinical Oncology. 1982 Oct;104(3):219–27. doi: 10.1007/bf00406242.